N6 -substituted adenosines and method of use

Claim 1

A compound of the formula ##STR6## or a pharmaceutically acceptable addition salt thereof, wherein R 1 is hydrogen or lower alkyl; Ar and Ar 1 are each independently phenyl, phenyl substituted by halogen, hydroxy, thiol, lower alkoxy, lower thioalkoxy, lower alkanoyloxy, lower alkyl, nitro, amino, low S(O) n , -alkyl in which n is zero, one, or two, sulfonamide or trifluoromethyl, or 2-, 3-, or 4-pyridyl, 2- or 3-thienyl or -furanyl; A is straight or branched alkylene of one to eight carbon atoms which may be interrupted by oxygen, sulfur, or NH between two and seven carbons of the alkylene chain; X is hydrogen, hydroxy, lower alkyl, lower carboalkoxy, or lower alkanoyloxy; Y is hydrogen, halogen, --NR 2 R 3 , --OR 2 , or --SR, in which R 2 and R 3 are independently hydrogen, lower alkyl or phenyl lower alkyl; Z is hydrogen or halogen; R 2 ' and R 3 ' are each independently hydrogen, alkanoyl having two to twelve carbon atoms in a straight or branched alkyl chain which may be substituted by amino, benzoyl or benzoyl substituted by lower alkyl, lower alkoxy, halogen, or trifluoromethyl; R 2 ' and R 3 ' may be linked together to form a five-membered alkylidene ring having a total of up to 20 carbons, and R 5 ' is hydrogen; alkanoyl having two to twelve carbons in a straight or branched alkyl chain which may be substituted by amino, benzoyl or benzoyl substituted by lower alkyl, lower alkoxy, halogen, or trifluromethyl; phosphate; hydrogen phosphate; dihydrogen phosphate; an alkali or dialkali or dialkali metal phosphate; with the overall proviso that A cannot be a branched alkylene of two to eight carbon atoms.

Claim 14

A method for treating psychosis in a mammal suffering therefrom comprising administering an anti psychotic effective amount to such mammal a compound of the formula ##STR7## or a pharmaceutically acceptable addition salt thereof, wherein R 1 is hydrogen or lower alkyl; Ar and Ar 1 are each independently phenyl phenyl substituted by halogen, hydroxy thiol, lower alkoxy, lower thioalkoxy, lower alkanoyloxy, lower alkyl, nitro, amino, lower S(O) n -alkyl in which n is zero, one, or two, sulfonamide or trifluromenthyl, or 2-, 3-, or 4-pyridyl, 2- or 3-thienyl or -furanyl; A is straight or branched alkylene of one to eight carbon atoms which may be interrupted by oxygen, sulfur, or NH between two and seven carbons of the alkylene chain; X is hydrogen, hydroxy, lower alkyl, lower carboalkoxy, or lower alkanoyloxy; Y is hydrogen, halogen, --NR 2R 3, --OR 2, or --SR 2 in which R 2 and R 3 are independently hydrogen, lower alkyl or phenyl lower alkyl; Z is hydrogen or halogen; R 2 ' and R 3 ' are each independently hydrogen, alkanoyl having two to twelve carbon atoms in a straight or branched alkyl chain which may be substituted by amino, benzoyl or benzoyl substituted by lower alkyl, lower alkoxy, halogen, or trifluromethyl; R 2 ' and R 3 ' may be linked together to from a five-membered alkylidene ring having a total up to 20 carbons, and R 5 ' is hydrogen, alkanoyl having two to twelve carbons in a straight or branched alkyl chain which may be substituted by amino, benzoyl or benzoyl substituted by lower alkyl; lower alkoxy, halogen, or trifluromethyl; phosphate; hydrogen phosphate; dihydrogen phosphate; an alkali or dialkali metal phosphate; ammonium or diammonium phosphate; with the overall proviso that A cannot be a branched alkylene of two to eight carbon atoms in unit dosage forms.

Claim 15

A method for treating psychosis in a mammal suffering therefrom comprising administering an anti psychotic effective amount to such mammal a compound of the formula ##STR7## or a pharmaceutically acceptable addition salt thereof, wherein R 1 is hydrogen or lower alkyl; Ar and Ar 1 are each independently phenyl phenyl substituted by halogen, hydroxy thiol, lower alkoxy, lower thioalkoxy, lower alkanoyloxy, lower alkyl, nitro, amino, lower S(O) n -alkyl in which n is zero, one, or two, sulfonamide or trifluromenthyl, or 2-, 3-, or 4-pyridyl, 2- or 3-thienyl or -furanyl; A is straight or branched alkylene of one to eight carbon atoms which may be interrupted by oxygen, sulfur, or NH between two and seven carbons of the alkylene chain; X is hydrogen, hydroxy, lower alkyl, lower carboalkoxy, or lower alkanoyloxy; Y is hydrogen, halogen, --NR 2R 3, --OR 2, or --SR 2 in which R 2 and R 3 are independently hydrogen, lower alkyl or phenyl lower alkyl; Z is hydrogen or halogen; R 2 ' and R 3 ' are each independently hydrogen, alkanoyl having two to twelve carbon atoms in a straight or branched alkyl chain which may be substituted by amino, benzoyl or benzoyl substituted by lower alkyl, lower alkoxy, halogen, or trifluromethyl; R 2 ' and R 3 ' may be linked together to from a five-membered alkylidene ring having a total up to 20 carbons, and R 5 ' is hydrogen, alkanoyl having two to twelve carbons in a straight or branched alkyl chain which may be substituted by amino, benzoyl or benzoyl substituted by lower alkyl; lower alkoxy, halogen, or trifluromethyl; phosphate; hydrogen phosphate; dihydrogen phosphate; an alkali or dialkali metal phosphate; ammonium or diammonium phosphate; with the overall proviso that A cannot be a branched alkylene of two to eight carbon atoms in unit dosage forms.